Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T30420 | Target Info | |||
| Target Name | SET domain containing 8 (KMT5A) | ||||
| Synonyms |
SETD8; SET8; SET07; SET domain-containing protein 8; PRSET7; PR/SET07; PR/SET domain-containing protein 07; PR-Set7; N-lysine methyltransferase KMT5A; Lysine-specific methylase 5A; Lysine N-methyltransferase 5A; Histone-lysine N-methyltransferase KMT5A; H4-K20-HMTase KMT5A
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|
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| Target Type | Preclinical Target | ||||
| Gene Name | KMT5A | ||||
| Biochemical Class | Methyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(5-Pyrrolizinopentyl)-2-pyrrolizino-6-methoxyquinazoline-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622289; BDBM50498716
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| Activity |
IC50 = 52000 nM
|
[1] | |||
| Compound Name |
5-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-1-pyrrolidin-1-ylpentan-1-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318297; BDBM50051129
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|
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| Activity |
IC50 = 58000 nM
|
[2] | |||
| Compound Name |
N-(5-Pyrrolizinopentyl)-2-pyrrolizino-6-isopropoxy-7-methoxyquinazoline-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622291; BDBM50498735
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| Activity |
IC50 = 61000 nM
|
[1] | |||
| Compound Name |
N-[2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]ethyl]-2-pyrrolidin-1-ylacetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622267; BDBM50498726
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|
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| Activity |
IC50 = 63000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-pyrrolidin-1-yl-N-(2-pyrrolidin-1-ylethyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318286; BDBM50051118
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|
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| Activity |
IC50 = 67000 nM
|
[2] | |||
| Compound Name |
6,7-Dimethoxy-2-piperidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318299; BDBM50051131
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|
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| Activity |
IC50 = 94000 nM
|
[2] | |||
| Compound Name |
2-(3,3-Difluoroazetidin-1-yl)-6,7-dimethoxy-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622270; BDBM50498729
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|
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| Activity |
IC50 = 110000 nM
|
[1] | |||
| Compound Name |
N-(5-Pyrrolizinopentyl)-2-pyrrolizino-6-methoxy-7-(benzyloxy)quinazoline-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621699; BDBM50498719
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|
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| Activity |
IC50 = 130000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 30 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
6,7-Dimethoxy-2-N-methyl-2-N,4-N-bis(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622275; BDBM50498708
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-N-methyl-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318298; BDBM50051130
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
6,7-Dimethoxy-2-N-(4-nitrophenyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622282; BDBM50498697
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-N-Cyclohexyl-6,7-dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318307; BDBM50051390
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
N-(5-Pyrrolizinopentyl)-2-pyrrolizino-7-methoxyquinazoline-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622288; BDBM50498733
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-piperazin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318302; BDBM50051134
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
6,7-Dimethoxy-2-N-(4-methoxyphenyl)-2-N-methyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622277; BDBM50498707
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-(4-methylpiperazin-1-yl)-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318303; BDBM50051239
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
2-N-(4-Fluorophenyl)-6,7-dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622286; BDBM50498732
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-N-phenyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622279; BDBM50498705
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-(Azepan-1-yl)-6,7-dimethoxy-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318300; BDBM50051132
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
N-(5-Pyrrolizinopentyl)-2-pyrrolizinoquinazoline-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622287; BDBM50498715
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-N-[2-(4-methylpiperazin-1-yl)ethyl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621705; BDBM50498701
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-N-(2-pyrrolidin-1-ylethyl)acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622268; BDBM50498711
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-N-(4-methoxyphenyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622280; BDBM50498723
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-N-(5-pyrrolidin-1-ylpentyl)-2-[4-(trifluoromethyl)phenyl]quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622285; BDBM50498702
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
4-N-(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)cyclohexane-1,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622265; BDBM50498712
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-Chloro-6,7-dimethoxy-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318308; BDBM50051398
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
6,7-Dimethoxy-2-N-methyl-2-N-(2-pyrrolidin-1-ylethyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622272; BDBM50498736
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
N-[4-(Aminomethyl)cyclohexyl]-6,7-dimethoxy-2-pyrrolidin-1-ylquinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622266; BDBM50498699
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-(4-methoxyphenyl)-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622284; BDBM50498703
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-N-Cyclopentyl-6,7-dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3318306; BDBM50051387
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|
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| Activity |
IC50 > 250000 nM
|
[2] | |||
| Compound Name |
N-(5-Pyrrolizinopentyl)-2-pyrrolizino-6-methoxy-7-hydroxyquinazoline-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3621700; BDBM50498695
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-4-N-(5-pyrrolidin-1-ylpentyl)-2-N-[4-(trifluoromethyl)phenyl]quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622281; BDBM50498704
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-N-methyl-2-N-phenyl-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622276; BDBM50498724
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
2-[(6,7-Dimethoxy-2-pyrrolidin-1-ylquinazolin-4-yl)amino]-N-(2-piperazin-1-ylethyl)acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622269; BDBM50498710
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-phenyl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622283; BDBM50498728
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-N-methyl-2-N-(4-pyrrolidin-1-ylbutyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622274; BDBM50498698
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-N-methyl-2-N-(4-nitrophenyl)-4-N-(5-pyrrolidin-1-ylpentyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622278; BDBM50498706
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Compound Name |
6,7-Dimethoxy-2-N-methyl-4-N-(5-pyrrolidin-1-ylpentyl)-2-N-(3-pyrrolidin-1-ylpropyl)quinazoline-2,4-diamine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3622273; BDBM50498709
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|
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| Activity |
IC50 > 250000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-activity relationship studies of SETD8 inhibitors. Medchemcomm. 2014 Dec;5(12):1892-1898. | ||||
| REF 2 | Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33. | ||||
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